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Progettazione, sintesi e attività anti-HIV degli analoghi della curcumina by Mohamed Jawed Ahsan, Sachin Kumar Sharma

Progettazione, sintesi e attività anti-HIV degli analoghi della curcumina

by Mohamed Jawed Ahsan , Sachin Kumar Sharma
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Book cover type: Paperback
  • ISBN13: 9786209358456
  • Binding: Paperback
  • Subject: N/A
  • Publisher: Edizioni Sapienza
  • Publisher Imprint: Edizioni Sapienza
  • Publication Date:
  • Pages: 56
  • Original Price: GBP 34.71
  • Language: Italian
  • Edition: N/A
  • Item Weight: 87 grams
  • BISAC Subject(s): Pharmacology

Una serie di 11 analoghi della curcumina � stata sottoposta a previsione delle propriet� molecolari e somiglianza farmacologica mediante i software Molinspiration e MolSoft, nonch� a parametri di lipofilia e solubilit� utilizzando il programma ALOGPS 2.1. I composti che seguivano la "Regola dei cinque" di Lipinski sono stati sintetizzati per lo screening anti-HIV come farmaci/principi attivi biodisponibili per via orale. Successivamente, la struttura dei composti sintetizzati � stata confermata da analisi spettrali (IR, NMR e massa) e i composti (3a-k) sono stati valutati per l'attivit� anti-HIV secondo il protocollo standard. Il punteggio massimo del modello di somiglianza farmacologica (1.1.0) � stato riscontrato per il 3,5-bis(4-idrossi-3-metilstiril)-N-(4-clorofenil)-1H-pirazolo-1-carbossamide (3b). Il composto 3b ha dimostrato attivit� anti-HIV con IC50 >3,71 M e CC50 3,71 M, tuttavia l'attivit� � risultata inferiore a quella del farmaco standard zidovudina.

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